반응 #220702

반응 방정식

3-(4-fluoro-phenyl)-3-oxo-propionitrile

[1,4]dithiane-2,5-diol

diethyl-amine

→

(2-amino-thiophen-3-yl)-(4-fluoro-phenyl)-methanone

수율 86.2%

용매

ethanol

반응 조건

후처리

1. 1
   workup.ADDITIONwere charged in a sealed tube
2. 2
   기타was then placed in a fridge (about 4° C.) for the night
3. 3
   여과the product was collected by filtration
4. 4
   기타dried under vacuum

실험 절차

Following a procedure described in J. Med. Chem. 2002, 45, 382-389; 0.44 g (2.7 mmol) 3-(4-fluoro-phenyl)-3-oxo-propionitrile (the preparation of which is described in example 17), 0.33 g (2.15 mmol) [1,4]dithiane-2,5-diol, 0.16 ml (2.15 mmol) diethyl-amine and 5 ml ethanol were charged in a sealed tube. The reaction mixture was heated at 50° C. for 6 h. The tube was then placed in a fridge (about 4° C.) for the night, and the product was collected by filtration and dried under vacuum to afford 0.41 g (69%) (2-amino-thiophen-3-yl)-(4-fluoro-phenyl)-methanone as a light brown crystals.

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